Abstract: Processes for preparing oxycodone are provided. Said processes encompass a step which is a hydrogenation of an 14-hydroxycodeinone salt in the presence of trifluoroacetic acid and/or a glycol.

Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: Numerous diseases have been linked to the production of effector cells. The present invention relates to the realization that effector cells are cycling in these diseases. In addition, the present invention relates to the determination that regulator cells are cycling in degenerative diseases. Based on these realizations, the present invention provides methods for treating conditions such as autoimmune diseases, degenerative diseases, and graft-versus-host disease. The present invention also relates to methods of determining when therapy should be administered to a patient.

Abstract: The present invention provides processes for preparing nal-opiates without the isolation of intermediates. In general, the process provides for alkylation and reduction in the same pot to give the nal-opiate.

Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein , R1a—R3a, R4, Y and Za are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.

Abstract: A pseudorotaxane, a rotaxane and a catenane are provided. The pseudorotaxane includes at least a macrocyclic host molecule, a guest molecule, and a metal ion. The host molecule contains at least a binding unit and an aromatic linking spacer. The guest molecule has at least a recognition unit. The metal ion is used to template the threading of the guest molecule through the macrocycle host molecule by coordinating to a binding pocket formed from the binding unit of the macrocycle and the recognition moiety of the guest molecule. Rotaxanes or catenanes can be synthesized from the pseudorotaxane complexes, with or without the metal template ion in their molecular structures.

Abstract: The present invention relates to compounds of the formula (1) and formula (2) which are suitable for use in electronic devices, in particular organic electroluminescent devices.

Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein , R1a, R3a, R4, Y and Za are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.

Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein Cy, R1a-R3a, R4a, and R4b are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.

Abstract: Novel compounds which are alkaloids related to bis [O-(14-Benzoylaconine-8-YL)]esters.

Abstract: A (+)-3-hydroxymorphinan-based polycycle derivative of formula (I) is effective as a neuroprotective agent for neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, and ischemic stroke.

Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.

Abstract: The resolution of racemic 1-(4-methoxybenzyl)-octahydro-isoquinoline, a key intermediate in the synthesis of the antitussive agent dextromethorphan, is reported using (R)-2-(6-methoxy-2-naphthyl) propionic acid in good yields. The resolving agent and the undesired isomer of the octahydro-isoquinoline have been recovered in good yield.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: The invention generally provides processes and intermediate compounds useful for the production of (+) nal morphinan compounds. In particular, the process encompasses synthetic routes for the production of (+) nal morphinan compounds or derivatives of (+) nal morphinan compounds from (+)-morphinan substrates such as (+)-hydrocodone, (+)-norhydrocodone or derivatives of either compound.

Abstract: There is provided an organic light-emitting device having an optical output with a high efficiency and a high luminance, and having good durability. The organic light-emitting device includes an anode, a cathode, and a layer including an organic compound interposed between the anode and the cathode, in which the layer contains a naphthalene compound represented by the general formula (1): wherein Ar1's each represent a substituted or unsubstituted fused ring aromatic hydrocarbon group having four or more rings.

Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract: The present invention provides processes for the synthesis of five and six membered rings. In particular, the present invention provides processes for the synthesis of five and six membered rings in alkaloids.

Abstract: The present invention provides a synthetic process for the N-demethylation of N-methyl morphinans. In particular, the invention provides improved synthetic methods for the preparation of N-demethylated morphinan compounds that may be employed as starting materials, for example, commonly available N-methyl opiates such as oripavine and thebaine, and C(3)-protected hydroxy derivatives of oripavine.

Abstract: There is provided an organic light-emitting device having an optical output with a high a high efficiency and a high luminance, and having good durability. The organic light-emitting device includes an anode, a cathode, and a layer including an organic compound interposed between the anode and the cathode, in which the layer contains a naphthalene compound represented by the general formula (1): wherein Ar1's each represent a substituted or unsubstituted fused ring aromatic hydrocarbon group having four or more rings.

Abstract: This invention features opioid compounds having activity at kappa and mu receptors, methods for preparing the mu/kappa opioids, and methods for the treatment of pain or a dopamine dysregulation disease, such as schizophrenia, attention deficit hyperactivity disorder (ADHD), attention deficit hyperactivity disorder (ADD), Parkinson's disease, hyperprolactinemia, depression, and addiction.

Abstract: Photochromic 3H-naphtho[2,1-b]pyran compounds corresponding to formula I in which the groups R1 to R7 and B? have defined meanings and the use of such photochromic compounds in synthetic resin articles of all types, particularly for ophthalmic purposes. The photochromic 3H-naphtho[2,1-b]pyran derivatives have particularly long-waved absorption maxima in the open form, and when used in photochromic eyeglass lenses, produce essentially blue color tones which have a high darkening capacity.

Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: Novel haptens, which can be conjugated to form immunogens, are of formula I, II or III wherein R is a divalent alkyl, cycloalkyl or aryl group having 1 to 10 carbon atoms, and X is a functional group.

Abstract: A morphine component, e.g., a concentrate of poppy straw, is converted into codeine in high yield and high purity and in a highly controlled manner. The conversion process involves the following steps: (a) providing a solution or suspension of a morphine component in an inert solvent or a mixture of solvents; (b) methylating the resultant solution or suspension with a methylating agent in the presence of an alkaline ingredient; and (c) recovering the resultant codeine as the free base or as a salt.

Abstract: A morphine component, e.g., a concentrate of poppy straw, is converted into codeine in high yield and high purity and in a highly controlled manner. The conversion process involves the following steps: (a) providing a solution or suspension of a morphine component in an inert solvent or a mixture of solvents; (b) methylating the resultant solution or suspension with a methylating agent in the presence of an alkaline ingredient; and (c) recovering the resultant codeine as the free base or as a salt.

Abstract: A process for the preparation of dihydrocodeine by hydrogenating codeine or a salt thereof in aqueous solution in the presence of a catalytic metal and deactivating agent that decreases impurities formation.

Abstract: Magenta ink exhibiting excellent coloration on various recording materials is provided according to the present invention. The magenta ink can realize high image densities and can produce images having superior light resistance.

Abstract: New derivatives of benzazepine, particularly of benzofuro[3a,3,2,ef][2]benzazepin of the general formula (I) 1

Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds. pharmaceutical compositions containing such compounds and methods of using such compounds, in the treatment of neurological and psychological disorders.

Abstract: Heterocycle-condensed morphinoid derivatives of formula (I), or solvates or salts thereof, are potent and selective delta opioid agonists and antagonists and are useful as i.a. analgesics. Pharmaceutical compositions containing such compounds, the use of such compounds as therapeutic agents, a method of treatment comprising the administration of such compounds, and a process for the preparation of such compounds are also described.

Abstract: Magenta ink exhibiting excellent coloration on various recording materials is provided according to the present invention. The magenta ink can realize high image densities and can produce images having superior light resistance. The magenta ink contains first and second coloring materials represented by the following general formulae 1 and 2, respectively, and a water-based medium.

Abstract: The nalbuphine polyester derivative is related to a novel long acting agent. The nalbuphine polyester derivative is R—[CO-NAL]n wherein n is an integer from 2-4 and, in which the R is selected from a saturated or nonsaturated, substituted or unsubstituted, aliphatic or aromatic group having 1 to 40 carbon atoms. The process for producing the derivative includes esterifying nalbuphine with a saturated or unsaturated fatty acid or a halogen compound of the fatty acid with an acid anhydride. A pharmaceutical composition contains the derivative and a pharmaceutically acceptable carrier, which can be administered to an animal or person for treating pain.

Abstract: The present invention provides imino aza-anthracyclinones and a method of treating amyloidoses using the same.

Abstract: Compounds of formula (I), are selective delta opioid agonsist and antagonists, and are useful as analgesics and in treating general neurologic disorders.

Abstract: Non-naturally occuring dynemicin analogs are provided, which are useful as DNA cleaving agents, cytotoxic agents, and/or anti-tumor compounds. Methods of making dynemicin analogs are also provided.

Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

Abstract: Non-naturally occuring dynemicin analogs are provided, which are useful as DNA cleaving agents, cytotoxic agents, and/or anti-tumor compounds. Methods of making dynemicin analogs are also provided.

Abstract: Disclosed are processes for resolving a racemic mixture of 5-aminocarbonyl-5H-dibenzo?a,d!cyclohepten-5,10-imines into component enantiomers comprising recrystallizaton of diasteriomeric tartrate salts.

Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: A quinone imine enediyne possessing cytotoxic activity towards cancer cells having the general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently the same or different and are H, Br, Cl, F, NH.sub.2, CO.sub.2 H, or OH or a linear or branched alkyl, etc.; wherein R.sub.4 is H, OH or a linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R.sub.5 is H, Br, Cl, F, O.dbd., OH or S--SR, or a linear or branched alkyl, etc.; wherein R.sub.6 is H, Br, Cl, F, CO.sub.2 H, OH or S--SR', or a linear or branched alkyl, etc; wherein R.sub.7 is H, OH or S--SR", or a linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl group; and wherein R, R' and R" are independently the same or different and are a linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl group.

Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.

Abstract: The invention relates to the method of synthesis of bicyclic hexahydroaporphine compounds which may provide improved therapy for diseases characterized by an increase in intraocular pressure. More specifically, the present invention relates to the preparation of agents which may provide for improved treatment of patients with glaucoma or ocular hypertension. The present invention describes the intraocular pressure lowering capabilities of several of the bicyclic hexahydroaporphine structures.

Abstract: 6,11'-Cyclyl-1,2,3,4,5,6,11,11a-octahydrobenzo[b]quinolizine derivatives, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: 6,11-Substituted-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: Polycyclic diamines, incorporating a basic framework similar to [3.3.3]propellane, and derivatives of the basic polycyclic diamines and a process for preparing same are provided. The diamines are prepared by subjecting bispyridine compounds to electroreductive coupling in an acidic solution. The polycyclic diamines and derivatives thereof are useful as chain extenders, crosslinking agents and curatives in various polymer systems.